Histogranin-like peptides and non-peptides, processes for...

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Peptide containing doai

Reexamination Certificate

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C514S002600, C514S018700, C530S300000, C530S317000, C530S321000, C530S331000

Reexamination Certificate

active

06972281

ABSTRACT:
The invention relates to new basic amino acid derivatives of general formula I and the preparation and use thereof in treatment of pain. The compounds have histogranin-like antinociceptive, morphine potentiating and COX-2 induction modulating activities.wherein:A is -hydrogen, —(C1-C8)alkyl or —(C1-C8)alkyl substituted by hydroxy;B is —(C1-C6)alkylguanidino, —(C1-C6)alkyl(4-imidazo-lyl), —(C1-C6)alkylamino, p-aminophenylalkyl(C1-C6)—, p-guanidinophenylalkyl(C1-C6)— or 4-pyridinylalkyl(C1-C6)—;R1, R2and R3are, independent of one another, -hydrogen, -arylcarbonylamino, —(C1-C6)alkoylamino, —(C1-C6)alkylamino, —(C1-C6)alkyloxy, —(C1-C6)alkylaminocarbonyl, -carboxy, —OH, -benzoyl, -p-halogenobenzoyl, -methyl, —S-(2,4-dinitrophenyl), —S-(3-nitro-2-pyridinesulfenyl), -sulfonyl, -trifluoromethyl, —(C1-C6)alkylaminocarbonylamino, -halo or -amino;R4and R5are, independent of one another, -hydrogen, —(C1-C6)alkyl, -methyloxy, -nitro, -amino, -arylcarbonylamino, —(C1-C6)alkoylamino, —(C1-C6)alkylamino, -halo or —OH.

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